Boltze K H, Kreisfeld H
Arzneimittelforschung. 1977;27(6B):1300-12.
Etofenamate is 2-(2-hydroxyethoxy)ethyl-N-(a,a,a,-trifluorom-tolyl)anthranilate and has been selected as an antiphlogistic agent for percutaneous therapy. Its characteristic alcohol-ether-ester structure brings about an increase in lipophilia and in its ability to penetrate through the intact skin. Furthermore, its oily consistency renders it ideal for pharmaceutical formulation in gels. The physico-chemical material constants, partition coefficients (RM values) as a measure for lipophilia, spectra and molecular models of etofenamate are described. Various methods of synthesis of etofenamate and of its intermediates are described. Structural identification is made of by-products simultaneously obtained in the reaction. Pure etofenamate is obtained through repeated molecular distillation. The synthesis is carried out uniformly with protected reaction components and, after splitting off the protective groups, extremely pure etofenamate is obtained.
依托芬那酯是2-(2-羟基乙氧基)乙基-N-(α,α,α-三氟间甲苯基)邻氨基苯甲酸酯，已被选作经皮治疗的抗炎剂。其独特的醇-醚-酯结构使其亲脂性增加，穿透完整皮肤的能力增强。此外，其油性稠度使其成为凝胶剂药物制剂的理想选择。描述了依托芬那酯的物理化学物质常数、作为亲脂性度量的分配系数（RM值）、光谱和分子模型。描述了依托芬那酯及其中间体的各种合成方法。对反应中同时得到的副产物进行了结构鉴定。通过反复分子蒸馏获得纯依托芬那酯。合成过程中使用受保护的反应组分统一进行，脱除保护基团后得到极纯的依托芬那酯。
